MPT0E028
CAS 1338320-94-7 MFCD438320947
化学结构图
SMILES: O=C(/C=C/c1ccc2c(c1)CCN2S(=O)(=O)c1ccccc1)NO
化学属性
| Mol. Weight | 344.38494 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | MPT0E028 |
|---|---|
| Formula | C17H16N2O4S |
| Synonym | MPT-0E028; MPT0E028; MPT 0E028 |
| IUPAC Name | (E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide |
| InChIKey | MGTIFSBCGGAZDB-VQHVLOKHSA-N |
| InChI | InChI=1S/C17H16N2O4S/c20-17(18-21)9-7-13-6-8-16-14(12-13)10-11-19(16)24(22,23)15-4-2-1-3-5-15/h1-9,12,21H,10-11H2,(H,18,20)/b9-7+ |
| Canonical SMILES | O=C(NO)/C=C/C1=CC2=C(N(S(=O)(C3=CC=CC=C3)=O)CC2)C=C1 |
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产品应用
- MPT0E028 is a novel N-hydroxyacrylamide-derived HDAC inhibitor, inhibited human colorectal cancer HCT116 cell growth in vitro and in vivo. The results of NCI-60 screening showed that MPT0E028 inhibited proliferation in both solid and hematological tumor cell lines at micromolar concentrations, and was especially potent in HCT116 cells. MPT0E028 had a stronger apoptotic activity and inhibited HDACs activity more potently than SAHA, the first therapeutic HDAC inhibitor proved by FDA. In vivo murine model, the growth of HCT116 tumor xenograft was delayed and inhibited after treatment with MPT0E028 in a dose-dependent manner. Based on in vivo study, MPT0E028 showed stronger anti-cancer efficacy than SAHA. No significant body weight difference or other adverse effects were observed in both MPT0E028-and SAHA-treated groups. Taken together, our results demonstrate that MPT0E028 has several properties and is potential as a promising anti-cancer therapeutic drug. ( PLoS One. 2012;7(8):e43645.)
